公开(公告)号：NO315424B1

公开(公告)日：2003-09-01

申请号：NO970697

申请日：1997-02-14

Applicant: HOECHST AG

Inventor： SCHWARK JAN-ROBERT ,  BRENDEL JOACHIM ,  KLEEMANN HEINZ-WERNER ,  LANG HANS-JOCHEN ,  WEICHERT ANDREAS ,  ALBUS UDO ,  SCHOLZ WOLFGANG

IPC: C07D333/24 ,  A61K31/38 ,  A61K31/381 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C279/22 ,  C07D333/02 ,  C07D333/34 ,  A61K31/155

Abstract: Thiophenylalkenylcarboxylic acid guanidide derivatives of formula (I) and their salts are new. at least one of R1-R3 = Op(CH2)sCqF2q+1, R40CO or R31SOk; and the others = H, F, Cl, Br, I, CN, OnaCmaH2ma+1 or OgaCraH2raR10; p = 0 or 1; s = 0-4; q = 1-8; k = 0-2; R40, R31 = 1-8C alkyl, 1-8C perfluoroalkyl, 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me or OMe) or NR41R42; R41,R42 = H, 1-4C alkyl or 1-4C perfluoroalkyl; or R41+R42 = (CH2)x in which a CH2 group may be replaced by O, S, NH, NMe or N-benzyl; x = 4 or 5; na = 0 or 1; ma = 0-8; ga = 0 or 1; ra = 0-4; R10 = 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me or OMe); R4, R5 = H, F, Cl, Br, I, CN, 1-8C alkyl, 1-8C perfluoroalkyl, 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me, OMe or NR14R15); R14, R15 = H, 1-4C alkyl or 1-4C perfluoroalkyl.

公开(公告)号：PL185757B1

公开(公告)日：2003-07-31

申请号：PL32032797

申请日：1997-06-03

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS ,  BRENDEL JOACHIM ,  KLEEMANN HEINZ-WERNER ,  LANG HANS JOCHEN ,  SCHWARK JAN-ROBERT ,  ALBUS UDO ,  SCHOLZ WOLFGANG

IPC: A61K31/165 ,  A01N1/02 ,  A01N47/44 ,  A61K31/155 ,  A61P3/00 ,  A61P3/06 ,  A61P7/04 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  C07C279/22 ,  C07C319/20 ,  C07C323/62 ,  A67K31/22

Abstract: Ortho-substituted benzoyl-guanidines of formula (I) and their salts are new: R = H; F; Cl; Br; I; CN; NO2; 1-8 C alkyl; 1-8 C alkoxy; 3-8 C cycloalkyl; 3-8 C cycloalkoxy; Xa-(CH2)b-(CF2)c-CF3; SR ; OR ; CR R R ; Ph, etc.;R or R = OCOR and the other = R ;R , R = H; 1-4C alkyl; 1-4C alkoxy; etc.;X = e.g. O; a = 0 or 1;b = 0-2;c = 0-3;R = -CfH2f-Q;Q = e.g. 3-8 C cycloalkyl;f = 0-2; R , R = H; 1-4 C alkyl; or R ; R = e.g. 1-8C alkyl.

公开(公告)号：PL185756B1

公开(公告)日：2003-07-31

申请号：PL32032697

申请日：1997-06-03

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS ,  BRENDEL JOACHIM ,  KLEEMANN HEINZ-WERNER ,  LANG HANS JOCHEN ,  SCHWARK JAN-ROBERT ,  ALBUS UDO ,  SCHOLZ WOLFGANG

IPC: A61K31/165 ,  A01N1/02 ,  A01N47/44 ,  A61K31/10 ,  A61K31/155 ,  A61K31/18 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C279/10 ,  C07C279/20 ,  C07C279/22 ,  C07C303/40 ,  C07C311/19 ,  C07C311/47 ,  C07C317/42 ,  C07C317/50 ,  C07C317/32

Abstract: Benzoylguanidine compounds of formula (I) and their salts are new. R1 = R13-SOm or R14R15N-SO2; m = 1 or 2; R13 = 1-8C alkyl or perfluoroalkyl, 3-8C alkenyl or CnH2n-R16; n = 0-4; R16 = 3-8C cycloalkyl or phenyl, biphenyl or naphthyl (each optionally substituted by 1-3 F, Cl, CF3, CH3, OCH3 or NR25R26); R25, R26 = H or 1-4C alkyl or perfluoroalkyl; R14 = H, 1-8C alkyl or perfluoroalkyl, 3-8C alkenyl or CnH2n-R27; R27 = 3-8C cycloalkyl or phenyl, biphenyl or naphthyl (each optionally substituted by 1-3 F, Cl, CF3, CH3, OCH3 or NR28R29); R28, R29, R15 = H, or 1-4C alkyl or perfluoroalkyl; or R14+R15 = (CH2)a where one CH2 group may be replaced by O, S, NH, N-CH3 or N-benzyl; a = 4-5; one of R2, R3 = H and the other = CHR30R31 or C(OH)R33R34; R30 = (CH2)g-(CHOH)h-(CH2)i-(CHOH)k-R32 or (CH2)g-O-(CH2-CH2O)h-R24; R24, R32 = H or Me; g, h, i = 0-4; k = 1-4; R31, R33, R34 = H or 1-4C alkyl; or R33+R34 = 3-6C cycloalkyl; or R33 = CH2OH; R4 = 1-4C alkyl or alkoxy or F, Cl, Br, I, CN, (CH2)n'-(CF2)o-CF3; n' = 0-1; and o = 0-2.

公开(公告)号：PL185751B1

公开(公告)日：2003-07-31

申请号：PL31841597

申请日：1997-02-11

Applicant: HOECHST AG

Inventor： ALBUS UDO ,  BRENDEL JOACHIM ,  KLEEMANN HEINZ-WERNER ,  LANG HANS JOCHEN ,  SCHOLZ WOLFGANG ,  SCHWARK JAN-ROBERT ,  WEICHERT ANDREAS

IPC: A01N1/02 ,  A61K31/155 ,  A61P3/10 ,  A61K31/165 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P25/00 ,  A61P35/00 ,  A61P43/00 ,  C07C279/10 ,  C07C279/20 ,  C07C279/22

Abstract: Ortho-substituted benzoyl-guanidines of formula (I) and their salts are new: where R1 = H, F, Cl, Br, I, CN, NO2, 1-8C alkyl, 1-8C alkoxy, 3-8C cycloalkyl, 3-8C cycloalkoxy, Xa-(CH2)b-(CF2)c-CF3, SR10, OR10, CR10R11R12; or phenyl, naphthyl, biphenylyl, or 1-9C (sic) heteroaryl bonded via C or N and all optionally mono- to tri-substituted with F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; or SR13, OR13, NHR13, NR13R14, CHR13R15, CR15R16-OH, C IDENTICAL CR18, CR19=CHR18, ÄCR20R21Ük-CO, ÄCR22R23Ül-R24; one of R2, R3 = hydroxy the other as R1; R4 = 1-4C alkyl, 1-4C alkoxy, F, Cl, Br, I or (CH2)n-(CF2)o-CF3; X = O, S, NR5; a = 0-1; b = 0-2; c = 0-3; R5 = H, 1-4C alkyl, CdH2d-R6; d = 0-4; R6 = 3-8C cycloalkyl; or phenyl, biphenylyl or naphthyl (each optionally mono- to tri-substituted with F, Cl, CF3, methyl, methoxy, or NR7R8); R7, R8 = H or 1-4C alkyl; R10 = CfH2f-3-8C cycloalkyl; or phenyl optionally mono- to tri-substituted with F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; f = 0-2; R11, R12 = as R10, H or 1-4C alkyl; k = 0-4; l = 0-4; R13, R14 = (CH2)g-(CHOH)h-(CH2)i-(CHOH)j-R17, or (CH2)g-O-(CH2CH2O)h-R24; R17 = H, CH3; g, h, i = 0-4; j = 1-4; R15, R16 = H or 1-6C alkyl; or CR15R16 = 3-8C cycloalkyl; R18 = phenyl optionally mono- to tri-substituted with F, Cl, CF3, CH3, OCH3 or NR25R26; or 3-8C cycloalkyl; or 1-9C (sic) heteroaryl optionally substituted as for phenyl; or 1-6C alkyl optionally substituted by 1-3 OH; R25, R26 = H or 1-4C alkyl; R19-R23 = H or CH3; R24 = H, 1-6C alkyl, 3-8C cycloalkyl, CmH2m-R18; m = 1-4; n = 0-1; and o = 0-1.

公开(公告)号：DK0847996T3

公开(公告)日：2003-06-30

申请号：DK97121437

申请日：1997-12-05

Applicant: HOECHST AG

Inventor： BRENDEL JOACHIM ,  LANG HANS JOCHEN ,  GERLACH UWE ,  WEIDMANN KLAUS

IPC: A61K31/33 ,  A61K31/35 ,  A61K31/352 ,  A61K31/44 ,  A61K31/4402 ,  C07D239/22 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/505 ,  A61K31/535 ,  A61K31/536 ,  A61K31/54 ,  A61K31/545 ,  A61P1/00 ,  A61P1/04 ,  A61P9/00 ,  A61P43/00 ,  C07D207/325 ,  C07D211/14 ,  C07D213/06 ,  C07D213/75 ,  C07D215/42 ,  C07D217/22 ,  C07D239/94 ,  C07D241/04 ,  C07D265/06 ,  C07D265/16 ,  C07D265/20 ,  C07D277/20 ,  C07D295/08 ,  C07D295/12 ,  C07D311/68 ,  C07D311/70 ,  C07D333/10 ,  C07D335/00 ,  C07D417/04

Abstract: N-(Bicyclic aryl or heteroaryl)-sulphonamide or sulphamide derivatives of formula (I) and their salts are new: X = O, S, SO, SO2, NR7, CR'8R"8 or C=O; R7 = H or -CaH2a-R9, where one CH2 is optionally replaced by O, CH=CH, C IDENTICAL C, CO, CO2, OCO, S, SO, SO2, NR10 or CONR10; R10 = H or A; a = 0-8; R9 = H, CF3, C2F5, C3F7, 3-8 C cycloalkyl, NMe2, NEt2, 1-piperidyl, pyrrolidino, morpholino or 4-methyl-piperazin-1-yl, pyridyl, thienyl, imidazolyl or phenyl (the latter four all optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); or R1+R7 = bond; R'8 = H, CF3, C2F5, C3F7, 1-6 C alkyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R"8 = H, A, OR10, CO2R10 or COR10; R10 = H or A; or R'8+R1 or R"8+R1 = bond if Y = N; Y = N or CR11; R11 = H or A; R1, R2 = H, CF3, C2F5, C3F7, F, Cl, OMe, 1-6 C alkyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); or CR1R2 = 2-10 C alkylene chain; R3 = R12-CnH2n-N(R13)- or R12-CnH2n-, where one CH2 of CnH2n is optionally replaced by O, CO, S, SO, SO2 or R'10; R'10 = H, Me or Et; R12 = H, Me, 3-8 C cycloalkyl, CF3, C2F5 or C3F7; n = 0-10; R13 = H or 1-6 C alkyl; or R12+R13 = bond if n ≥ 3; or R3+R4 = 3-8 C alkylene chain, where one CH2 is optionally replaced by O, CO, S, SO, SO2 or NR'10; R4 = R14-CrH2r-, where one CH2 of CrH2r is optionally replaced by O, CH=CH, C IDENTICAL C, CO, CO2, OCO, S, SO, SO2, NR"10 or CONR"10; R"10 = H or A; R14 = Me, CF3, C2F5, C3F7, 3-8 C cycloalkyl, OH, CO2H, NR23R24, 1-piperidyl, 1-pyrrolidinyl, 4-morpholinyl or 4-methylpiperazin-1-yl, pyridyl, thienyl, imidazolyl or phenyl (the latter four all optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R23, R24 = H or A; or NR23R24 = (CH2)k, where one CH2 is optionally replaced by O, S, NH, NMe or N(CH2Ph); k = 4 or 5; r = 0-20; R5+R6 = -CR15=CR16CR17=CR18-, -CR15=CR16CR17=N-, -CR15=CR16N=CR18-, -CR15=N-CR17=N-, -CR15=NN=CR18-, -N=CR16CR17=N- or -SCR15=CR16-, all bonded in either direction; R15-R18 = H, F, Cl, Br, I, 1-5C alkyl, 3-8 C cycloalkyl, CN, CF3, C2F5, C3F7, N3, NO2, -Z-CsH2s-R22, thienyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); Z = O, CO, CO2, OCO, S, SO, SO2, SO2O, SO2NR'"10, NR'"10 or CONR'"10; R'"10 = H or A; s = 0-6; R22 = H, CF3, C2F5, C3F7, 3-8 C cycloalkyl, NR19R20, CO2R21, 1-piperidyl, 1-pyrrolidinyl, 4-morpholinyl or 4-methylpiperazin-1-yl, pyridyl, thienyl, imidazolyl, quinolyl, isoquinolyl or phenyl (the latter six all optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R19, R20 = H or A; or NR19R20 = (CH2)k, where one CH2 is optionally replaced by O, S, NH, NMe or N(CH2Ph); R21 = H or A; and A = 1-3 C alkyl; provided that Y is not CR11 if X = O.

公开(公告)号：HRP970081B1

公开(公告)日：2003-04-30

申请号：HRP970081

申请日：1997-02-13

Applicant: HOECHST AG

Inventor： SCHWARK JAN-ROBERT ,  BRENDEL JOACHIM ,  KLEEMANN HEINZ-WERNER ,  LANG HANS-JOCHEN ,  WEICHERT ANDREAS ,  ALBUS UDO ,  SCHOLZ WOLFGANG

IPC: C07D333/24 ,  A61K31/38 ,  A61K31/381 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C279/22 ,  C07D333/02 ,  C07D333/34

Abstract: Thiophenylalkenylcarboxylic acid guanidide derivatives of formula (I) and their salts are new. at least one of R1-R3 = Op(CH2)sCqF2q+1, R40CO or R31SOk; and the others = H, F, Cl, Br, I, CN, OnaCmaH2ma+1 or OgaCraH2raR10; p = 0 or 1; s = 0-4; q = 1-8; k = 0-2; R40, R31 = 1-8C alkyl, 1-8C perfluoroalkyl, 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me or OMe) or NR41R42; R41,R42 = H, 1-4C alkyl or 1-4C perfluoroalkyl; or R41+R42 = (CH2)x in which a CH2 group may be replaced by O, S, NH, NMe or N-benzyl; x = 4 or 5; na = 0 or 1; ma = 0-8; ga = 0 or 1; ra = 0-4; R10 = 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me or OMe); R4, R5 = H, F, Cl, Br, I, CN, 1-8C alkyl, 1-8C perfluoroalkyl, 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me, OMe or NR14R15); R14, R15 = H, 1-4C alkyl or 1-4C perfluoroalkyl.

公开(公告)号：AT234821T

公开(公告)日：2003-04-15

申请号：AT97121437

申请日：1997-12-05

Applicant: HOECHST AG

Inventor： BRENDEL JOACHIM ,  LANG HANS JOCHEN ,  GERLACH UWE ,  WEIDMANN KLAUS

IPC: C07D239/22 ,  A61K31/33 ,  A61K31/35 ,  A61K31/352 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/505 ,  A61K31/535 ,  A61K31/536 ,  A61K31/54 ,  A61K31/545 ,  A61P1/00 ,  A61P1/04 ,  A61P9/00 ,  A61P43/00 ,  C07D207/325 ,  C07D211/14 ,  C07D213/06 ,  C07D213/75 ,  C07D215/42 ,  C07D217/22 ,  C07D239/94 ,  C07D241/04 ,  C07D265/06 ,  C07D265/16 ,  C07D265/20 ,  C07D277/20 ,  C07D295/08 ,  C07D295/12 ,  C07D311/68 ,  C07D311/70 ,  C07D333/10 ,  C07D335/00 ,  C07D417/04

Abstract: N-(Bicyclic aryl or heteroaryl)-sulphonamide or sulphamide derivatives of formula (I) and their salts are new: X = O, S, SO, SO2, NR7, CR'8R"8 or C=O; R7 = H or -CaH2a-R9, where one CH2 is optionally replaced by O, CH=CH, C IDENTICAL C, CO, CO2, OCO, S, SO, SO2, NR10 or CONR10; R10 = H or A; a = 0-8; R9 = H, CF3, C2F5, C3F7, 3-8 C cycloalkyl, NMe2, NEt2, 1-piperidyl, pyrrolidino, morpholino or 4-methyl-piperazin-1-yl, pyridyl, thienyl, imidazolyl or phenyl (the latter four all optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); or R1+R7 = bond; R'8 = H, CF3, C2F5, C3F7, 1-6 C alkyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R"8 = H, A, OR10, CO2R10 or COR10; R10 = H or A; or R'8+R1 or R"8+R1 = bond if Y = N; Y = N or CR11; R11 = H or A; R1, R2 = H, CF3, C2F5, C3F7, F, Cl, OMe, 1-6 C alkyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); or CR1R2 = 2-10 C alkylene chain; R3 = R12-CnH2n-N(R13)- or R12-CnH2n-, where one CH2 of CnH2n is optionally replaced by O, CO, S, SO, SO2 or R'10; R'10 = H, Me or Et; R12 = H, Me, 3-8 C cycloalkyl, CF3, C2F5 or C3F7; n = 0-10; R13 = H or 1-6 C alkyl; or R12+R13 = bond if n ≥ 3; or R3+R4 = 3-8 C alkylene chain, where one CH2 is optionally replaced by O, CO, S, SO, SO2 or NR'10; R4 = R14-CrH2r-, where one CH2 of CrH2r is optionally replaced by O, CH=CH, C IDENTICAL C, CO, CO2, OCO, S, SO, SO2, NR"10 or CONR"10; R"10 = H or A; R14 = Me, CF3, C2F5, C3F7, 3-8 C cycloalkyl, OH, CO2H, NR23R24, 1-piperidyl, 1-pyrrolidinyl, 4-morpholinyl or 4-methylpiperazin-1-yl, pyridyl, thienyl, imidazolyl or phenyl (the latter four all optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R23, R24 = H or A; or NR23R24 = (CH2)k, where one CH2 is optionally replaced by O, S, NH, NMe or N(CH2Ph); k = 4 or 5; r = 0-20; R5+R6 = -CR15=CR16CR17=CR18-, -CR15=CR16CR17=N-, -CR15=CR16N=CR18-, -CR15=N-CR17=N-, -CR15=NN=CR18-, -N=CR16CR17=N- or -SCR15=CR16-, all bonded in either direction; R15-R18 = H, F, Cl, Br, I, 1-5C alkyl, 3-8 C cycloalkyl, CN, CF3, C2F5, C3F7, N3, NO2, -Z-CsH2s-R22, thienyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); Z = O, CO, CO2, OCO, S, SO, SO2, SO2O, SO2NR'"10, NR'"10 or CONR'"10; R'"10 = H or A; s = 0-6; R22 = H, CF3, C2F5, C3F7, 3-8 C cycloalkyl, NR19R20, CO2R21, 1-piperidyl, 1-pyrrolidinyl, 4-morpholinyl or 4-methylpiperazin-1-yl, pyridyl, thienyl, imidazolyl, quinolyl, isoquinolyl or phenyl (the latter six all optionally substituted by 1 or 2 F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R19, R20 = H or A; or NR19R20 = (CH2)k, where one CH2 is optionally replaced by O, S, NH, NMe or N(CH2Ph); R21 = H or A; and A = 1-3 C alkyl; provided that Y is not CR11 if X = O.

公开(公告)号：RU2190601C2

公开(公告)日：2002-10-10

申请号：RU96115333

申请日：1996-07-25

Applicant: HOECHST AG

Inventor： SCHWARK JAN-ROBERT ,  BRENDEL JOACHIM ,  KLEEMANN HEINZ-WERNER ,  LANG HANS JOCHEN ,  WEICHERT ANDREAS ,  ALBUS UDO ,  SCHOLZ WOLFGANG

IPC: C07C279/20 ,  A01N1/02 ,  A61K31/155 ,  A61K31/16 ,  A61K31/275 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4418 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C277/08 ,  C07C279/22 ,  C07C323/62 ,  C07D213/65 ,  C07D213/70

公开(公告)号：PT754680E

公开(公告)日：2002-06-28

申请号：PT96111359

申请日：1996-07-15

Applicant: HOECHST AG

Inventor： UDO ALBUS DR ,  HEINZ-WERNER KLEEMANN DR ,  BRENDEL JOACHIM ,  HANS JOCHEN LANG DR ,  ANDREAS WEICHERT DR ,  SCHWARK JAN-ROBERT ,  SCHOLZ WOLFGANG

IPC: A01N1/02 ,  A61K31/155 ,  A61K49/00 ,  A61K31/165 ,  A61K31/18 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P41/00 ,  C07C303/40 ,  C07C311/16 ,  C07C315/04 ,  C07C317/44

Abstract: Benzoyl-guanidine derivs. of formula (I) and their salts are new: R1 = R4-SOm, R5R6N-SO2-, -Op-(CH2)q-(CF2)r-CF3, -SR10, -OR10 or -CR10R11R12; m = 1-2; R4, R5 = 1-8C alkyl, 3-6C alkenyl, CF3 or -CnH2n-R7; n = 0-4; R6 = H or 1-4C alkyl; R7 = 3-8C cycloalkyl or Ph (opt. substd. with 1-3 substits. from F, Cl, CF3, Me, OMe and NR8R9; R8, R9 = H or 1-4C alkyl; R5 = H; or R5 + R6 = 4-5C methylene group (with opt. replacement of a CH2 by O, S, NH, NMe or N-benzyl; ; p = 0-1; q = 0-2; r = 0-3;R10, R11, R12 = H, 1-8C alkyl, CsH2s-(3-8C cycloalkyl) or an aromatic gp. chosen from pyridyl, pyrrolyl, quinolyl, isoquinolyl, imidazolyl or Ph (in which the aromatic system may be opt. 1-3 times substd. by F, Cl, CF3, Me, OMe, OH, NH2, NHMe or N(Me)2; s = 0-2; R2 = -(CH2)u-(CF2)t-CF3; t = 0-3; u = 0-1; R3 = H or as for R1.

公开(公告)号：PT811610E

公开(公告)日：2002-05-31

申请号：PT97108258

申请日：1997-05-22

Applicant: HOECHST AG

Inventor： WOLFGANG SCHOLZ DR ,  UDO ALBUS DR ,  BRENDEL JOACHIM ,  HEINZ-WERNER KLEEMANN DR ,  HANS JOCHEN LANG DR ,  ANDREAS WEICHERT DR ,  SCHWARK JAN-ROBERT

IPC: A61K31/165 ,  A01N1/02 ,  A01N47/44 ,  A61K31/155 ,  A61P3/00 ,  A61P3/06 ,  A61P7/04 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  C07C279/22 ,  C07C319/20 ,  C07C323/62

Abstract: Ortho-substituted benzoyl-guanidines of formula (I) and their salts are new: R = H; F; Cl; Br; I; CN; NO2; 1-8 C alkyl; 1-8 C alkoxy; 3-8 C cycloalkyl; 3-8 C cycloalkoxy; Xa-(CH2)b-(CF2)c-CF3; SR ; OR ; CR R R ; Ph, etc.;R or R = OCOR and the other = R ;R , R = H; 1-4C alkyl; 1-4C alkoxy; etc.;X = e.g. O; a = 0 or 1;b = 0-2;c = 0-3;R = -CfH2f-Q;Q = e.g. 3-8 C cycloalkyl;f = 0-2; R , R = H; 1-4 C alkyl; or R ; R = e.g. 1-8C alkyl.